阿卡地新磷酸盐作用机制 - Medchemexpress - MCE中国

1、Product Data SheetAICAR phosphateCat. No.: HY-13417ACAS No.: 681006-28-0分式: CHNOP分量: 356.23作靶点: AMPK; Autophagy; Mitophagy作通路: Epigenetics; PI3K/Akt/mTOR; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 H2O : 180 mg/mL (505.29 mM)DMSO : 75 mg/mL (210.54 mM)*

2、means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 2.8072 mL 14.0359 mL 28.0718 mL5 mM 0.5614 mL 2.8072 mL 5.6143 mL10 mM 0.2807 mL 1.4036 mL 2.8072 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，

3、-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.84 mM); Clear solution此案

4、可获得 2.08 mg/mL (5.84 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 20.8 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.84 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.08 mg/mL (5.84 mM，饱和度

5、未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 20.8 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.84 mM); Clear solution此案可获得 2.08 mg/mL (5.84 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 20.8 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTI

6、VITY物活性 AICAR phosphate (Acadesine phosphate)种腺苷类似物，也 种 AMPK 激活剂。AICAR phosphate 调节葡萄糖和脂质的代谢，并抑制促炎细胞因和 iNOS 的产。AMPK 激活剂。IC & Target AMPK Autophagy Mitophagy体外研究 HepG2 cells are treated with various concentrations of AICAR (0.1-1.0 mM) for 12, 24, and 48 h, respectively. Theexpression level of IR- si

7、gnificantly decreases with 0.25, 0.5, and 1.0 mM of AICAR at 48 h to 50%, 53%, and 46% ofthe control, respectively1.体内研究 Fourteen-week-old male, lean (L; 31.3 g body wt) wild-type andob/ob (O; 59.6 g body wt) mice are injected with theAMP-activated kinase (AMPK) activator AICAR (A) at 0.5 mg*g body

8、wt-1*day-1 or saline control (C) for 14 days. At 24h after the last injection (including a 12-h fast), all mice are killed, and the plantar flexor complex muscle(gastrocnemius, soleus, and plantaris) is excised for analysis. Muscle mass is lower in OC (15912 mg) than LC, LA, andOA (17610, 1789, and

9、16616 mg, respectively) mice, independent of a body weight change3. The kidney weightis significantly higher in the untreated group when compared with both the exercise and AICAR (0.5 mg/g body wt)groups. The heart weight is higher in the exercise group than in the other groups, whereas the liver we

10、ight issignificantly higher in the AICAR-treated group when compared with the exercise and untreated groups4.PROTOCOLCell Assay 1 HepG2 cells (5105 cells) are plated in 6-well culture plate dishes and then are incubated in the serum-free media for12 h before transfection. One microgram of plasmid is

11、 transfected with FuGENE6 Transfection Reagent. After 5 h oftransfection, the culture media are removed and then media supplemented with or without AICAR (0.1-1.0 mM) areadded to each well. The stimulation media are changed every 24 h1.MCE has not independently confirmed the accuracy of these method

12、s. They are for reference only.Animal Mice2Administration 23 Fourteen-week-old lean (Lepob/+ or Lepob/+) and ob/ob (Lepob/Lepob/) male mice are uesd. After the 14-dayexperimental treatment (24 h after AICAR injection, including a 12-h fast), the plantar flexor complex muscle is cleanly(tendon-to-ten

13、don) excised from an anesthetized mouse. The muscle is quickly weighed and then processed forhistology or frozen in liquid nitrogen and stored at -80C. The anesthetized mice are killed by transection of thediaphragm and removal of the entire heart, after blood collection via needle puncture directly

14、 into the heart. AICARor saline (control) is injected subcutaneously into the lateral distal portion of the back. AICAR is administered at 0.5mg*g body wt-1*day-1 one time per day for 14 days. Saline (control) is injected in volumes identical to those used forAICAR treatment in a manner identical to

15、 that of AICAR treatment. Body weight is measured prior to death.Rats3Male 5-week-old ZDF rats are either subcutaneously injected with a single dose of AICAR (0.5 mg/g body wt) orPage 2 of 3 www.MedChemEunderwent a single bout of treadmill running (60 min, speed of 25 m/min at a 5% incline). Untreat

16、ed ZDF rats serveas controls (n=5 in each group). One hour after the subcutaneous AICAR injection or immediately after treadmillrunning, rats are killed by cervical dislocation. To avoid any effect of muscle spasm and hypoxia, red and whitegastrocnemius muscles are removed within seconds and immedia

17、tely freeze clamped for later determination ofAMPK activity.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Cell Metab. 2019 Jul 2;30(1):157-173.e7 Oncogene. 2019 Sep;38(38):6537-6549. Cell Death Dis. 2018 May 1;9(5):515. Arch Toxicol. 2019

18、Jun;93(6):1697-1712. J Cell Physiol. 2018 Dec;233(12):9701-9715.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Nakamaru K, et al. AICAR, an activator of AMP-activated protein kinase, down-regulates the IR expression in HepG2 cells. Biochem Biophys ResCommun. 2005 Mar 11;328(2):449-542. Drake JC, et al. AICAR treatment for 14 days normalizes obesity-induced dysregulation of TORC1 signaling and translational capacity in fasted skeletalmuscle. Am J Physi